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Desisobutyryl-ciclesonide

Cat. No. M13975
Desisobutyryl-ciclesonide Structure
Synonym:

CIC-AP; Ciclesonide active principle

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Biological Activity

Desisobutyryl-ciclesonide is the active metabolite of Ciclesonide. Desisobutyryl-ciclesonide has affinity for the glucocorticoid receptor.

Chemical Information
Molecular Weight 470.6
CAS Number 161115-59-9
Solubility (25°C) DMSO ≥ 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yu-Luan Chen, et al. An Ultrasensitive LC-APPI-MS/MS Method for Simultaneous Determination of Ciclesonide and Active Metabolite Desisobutyryl-Ciclesonide in Human Serum and Its Application to a Clinical Study

[2] Jatinder Kaur Mukker, et al. Ciclesonide: A Pro-Soft Drug Approach for Mitigation of Side Effects of Inhaled Corticosteroids

[3] Deepti Chopra, et al. Ciclesonide--a novel corticosteroid for the management of asthma

[4] Ruediger Nave, et al. Pharmacokinetics of ciclesonide and desisobutyryl ciclesonide after administration via aqueous nasal spray or hydrofluoroalkane nasal aerosol compared with orally inhaled ciclesonide: an open-label, single-dose, three-period crossover study in healthy vol䲧璵Ỵ璶

[5] Neil A Reynolds, et al. Ciclesonide

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Keywords: Desisobutyryl-ciclesonide, CIC-AP; Ciclesonide active principle supplier, GCR, inhibitors, activators


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